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NZ604379A - Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k - Google Patents

Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Info

Publication number
NZ604379A
NZ604379A NZ604379A NZ60437911A NZ604379A NZ 604379 A NZ604379 A NZ 604379A NZ 604379 A NZ604379 A NZ 604379A NZ 60437911 A NZ60437911 A NZ 60437911A NZ 604379 A NZ604379 A NZ 604379A
Authority
NZ
New Zealand
Prior art keywords
inhibitors
carboxamide
kinase p70s6k
bicyclic
quinazoline
Prior art date
Application number
NZ604379A
Inventor
Lizbeth Celeste Deselm
Bayard R Huck
Reinaldo C Jones
Srinivasa R Karra
Ruoxi Lan
Igor Mochalkin
Constantin Neagu
Thomas E Richardson
Amanda E Sutton
Yufang Xiao
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of NZ604379A publication Critical patent/NZ604379A/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Disclosed herein are bicyclic azaheterocyclic carboxamide compounds of formula (I) which are kinase P70S6K inhibitors useful in the treatment of hyperproliferative diseases, such as cancer. Embodiments of the compounds include the following: 4-{ [(1S)-1-(4-fluorophenyl)-2-(methylamino)ethyljamino} -2-methylquinazoline-8-carboxamide, 2-methyl-4-{ [(1S)-2-(methylamino)-1-phenylethyl]amino} quinazoline-8-carboxamide, and 4-[(S)-3-azetidin-1-yl-2-phenyl-propyl]-2-methyl-quinazoline-8-carboxylic acid amide.
NZ604379A 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k NZ604379A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29
PCT/EP2011/003272 WO2012013282A1 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Publications (1)

Publication Number Publication Date
NZ604379A true NZ604379A (en) 2015-01-30

Family

ID=44532723

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ604379A NZ604379A (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Country Status (18)

Country Link
US (1) US8710044B2 (en)
EP (1) EP2598492B1 (en)
JP (1) JP5894157B2 (en)
KR (1) KR101852644B1 (en)
CN (1) CN103003250B (en)
AR (1) AR082414A1 (en)
AU (1) AU2011285247B2 (en)
BR (1) BR112013002090A2 (en)
CA (1) CA2806610C (en)
CL (1) CL2013000263A1 (en)
EA (1) EA023132B1 (en)
ES (1) ES2557383T3 (en)
IL (1) IL224072A (en)
MX (1) MX2013001054A (en)
NZ (1) NZ604379A (en)
SG (1) SG187166A1 (en)
UA (1) UA110113C2 (en)
WO (1) WO2012013282A1 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
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US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
CA2797118C (en) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
ES2729754T3 (en) 2010-07-29 2019-11-06 Merck Patent Gmbh Azaheterocyclic carboxyamides of cyclic amines
PL2643313T3 (en) * 2010-11-24 2017-03-31 Merck Patent Gmbh Quinazoline carboxamide azetidines
SI2755958T1 (en) 2011-09-12 2017-12-29 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
SG10201606301YA (en) 2011-09-12 2016-09-29 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
ES2807539T3 (en) 2012-11-16 2021-02-23 Merck Patent Gmbh Imidazole-piperidinyl derivatives as modulators of kinase activity
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
ES2821102T3 (en) * 2012-11-29 2021-04-23 Merck Patent Gmbh Azaquinazolinecarboxamide derivatives
US9458134B2 (en) 2013-03-11 2016-10-04 Merck Patent Gmbh Heterocycles as modulators of kinase activity
CN103232401B (en) * 2013-04-12 2015-11-04 浙江工业大学 A kind of synthetic method of 4-arylthioquinazoline compound
CN103254141B (en) * 2013-04-26 2016-02-24 浙江工业大学 4-[4-(2-dipropyl aminoacetylamino) anilino]-6-substituted quinazoline compounds and Synthesis and applications
SG11201608189WA (en) 2014-04-03 2016-10-28 Merck Patent Gmbh Combinations of cancer therapeutics
CA2944140C (en) 2014-04-15 2022-10-04 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
US20230220395A1 (en) * 2020-04-21 2023-07-13 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
AU2021376892A1 (en) 2020-11-16 2023-06-29 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment
WO2023039068A1 (en) * 2021-09-08 2023-03-16 Neubase Therapeutics, Inc. Compositions and methods for synthesis of peptide nucleic acid intermediates

Family Cites Families (18)

* Cited by examiner, † Cited by third party
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GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
AR016817A1 (en) * 1997-08-14 2001-08-01 Smithkline Beecham Plc DERIVATIVES OF FENILUREA OR FENILTIOUREA, PROCEDURE FOR PREPARATION, COLLECTION OF COMPOUNDS, INTERMEDIARY COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT AND USE OF SUCH COMPOUNDS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT
JP3649395B2 (en) * 2000-04-27 2005-05-18 山之内製薬株式会社 Fused heteroaryl derivatives
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
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Also Published As

Publication number Publication date
CN103003250B (en) 2016-02-17
EA201300186A1 (en) 2013-12-30
AU2011285247A1 (en) 2013-03-14
MX2013001054A (en) 2013-02-21
EP2598492A1 (en) 2013-06-05
UA110113C2 (en) 2015-11-25
CN103003250A (en) 2013-03-27
US8710044B2 (en) 2014-04-29
CA2806610C (en) 2018-08-28
IL224072A0 (en) 2013-03-05
EP2598492B1 (en) 2015-10-28
WO2012013282A8 (en) 2012-03-29
ES2557383T3 (en) 2016-01-25
AU2011285247B2 (en) 2016-08-04
CA2806610A1 (en) 2012-02-02
HK1183302A1 (en) 2013-12-20
JP5894157B2 (en) 2016-03-23
WO2012013282A1 (en) 2012-02-02
US20130137677A1 (en) 2013-05-30
AR082414A1 (en) 2012-12-05
EA023132B1 (en) 2016-04-29
BR112013002090A2 (en) 2016-05-24
KR20130096714A (en) 2013-08-30
KR101852644B1 (en) 2018-04-26
IL224072A (en) 2016-02-29
JP2013532668A (en) 2013-08-19
CL2013000263A1 (en) 2013-09-06
SG187166A1 (en) 2013-02-28

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